This trial suggests ARQ531 could be an effective therapeutic option for patients with relapsed or refractory B cell malignancies, including BTK. ARQ 531 is presently being evaluated in an open-label, multicenter phase 1/2 trial in patients with a number of B-cell malignancies, including CLL (NCT03162536). You can follow us on Twitter and LinkedIn. ARQ 531 at 65 mg daily showed manageable safety profiles and significant anti-tumor efficacy therefore, 65 mg daily was determined as the recommended phase 2 dose in patients with B cell malignancies. ArQule's current discovery efforts are focused on the identification and development of novel kinase inhibitors, leveraging the Company's proprietary library of compounds. In addition, we have advanced ARQ 531, an investigational, orally bioavailable, potent and reversible inhibitor of both wild type and C481S-mutant BTK, in phase 1 for patients with B-cell malignancies refractory to other therapeutic options. ArQule's proprietary pipeline includes: ARQ 087, a multi-kinase inhibitor designed to preferentially inhibit the fibroblast growth factor receptor (FGFR) family, in phase 2 for iCCA and in phase 1b for multiple oncology indications ARQ 092, a selective inhibitor of the AKT serine/threonine kinase, in a phase 1/2 company sponsored study for Overgrowth Diseases, in a phase 1 study for ultra-rare Proteus syndrome conducted by the National Institutes of Health (NIH), as well as in multiple oncology indications ARQ 751, a next generation AKT inhibitor, in phase 1 for patients with AKT1 and PI3K mutations and ARQ 761, a β-lapachone analog being evaluated as a promoter of NQO1-mediated programmed cancer cell necrosis, in phase 1/2 in multiple oncology indications in partnership with the University of Texas Southwestern Medical Center. Our clinical-stage pipeline consists of five drug candidates, all of which are in targeted, biomarker-defined patient populations, making ArQule a leader among companies our size in precision medicine. against germinal center B-cell like subset of DLBCL cells (SU-DHL-4) compared with ARQ 531. inhibition by ARQ 531 ( IC50 1. ArQule's mission is to discover, develop and commercialize novel small molecule drugs in areas of high unmet need that will dramatically extend and improve the lives of our patients. ApCenterWatch Staff ArQule has received clearance from the FDA for the Investigational New Drug (IND) application to conduct a phase I clinical trial with ARQ 531 in patients with B-cell malignancies who are refractory to other therapeutic options. ARQ 531), another BTK C481S inhibitor in development. ArQule is a biopharmaceutical company engaged in the research and development of targeted therapeutics to treat cancers and rare diseases. ARQ 531 is a reversible non-covalent inhibitor of Brutons Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
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